119431-25-3

N-Methyl-D-aspartate (NMDA) receptors are calcium permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. Eliprodil is a non-competitive NMDA receptor antagonist that inhibits neuronal calcium channel currents. It is selective for NR2B subunit-containing receptors (IC₅₀ = 1 μM), displaying greater than 100-fold selectivity for NR2B over NR2A and NR2C subunits. Eliprodil also avidly binds σ₁ and σ₂ sites (K_is = 0.013 and 0.63 μM, respectively). It is effective in vivo, blocking ischemia-induced neurodegeneration in the CA1 region of the hippocampus of gerbils subjected to bilateral carotid artery occlusion. Eliprodil can also have proarrhythmic actions in hearts under normal conditions.

Eliprodil is a noncardiac drug with neuroprotective properties. It is also a N-Methyl-D-aspartate receptor (NMDAR) antagonist.

ChEBI: Eliprodil is a racemate comprising equimolar amounts of (R)- and (S)-eliprodil. It is a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist and an anti-ischaemic agent that exhibits neuroprotective properties. It has a role as a geroprotector, a NMDA receptor antagonist, a neuroprotective agent and a calcium channel blocker. It contains a (R)-eliprodil and a (S)-eliprodil.

Non-competitive NMDA receptor antagonist that acts at the polyamine modulatory site. Selective for NR2B- over NR2A- and NR2C-containing receptors (IC 50 values are 1, > 100 and > 100 μ M respectively). Also σ 1 ligand (K i = 0.013 μ M). Antagonizes neuronal voltage-gated Ca 2+ channels and selectively inhibits the rapid component of the delayed rectifier K + current (I Kr ). Neuroprotective.

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